Methods

MG85 complex was encapsulated into liposomal formulation with and without an active targeting moiety and cancer and healthy cells cytotoxicity was evaluated.

Results

Encapsulation of MG85 complex in targeting PEGylated liposomes enhanced colorectal carcinoma (HCT116) cancer cell death when compared to free complex, whilst decreasing cytotoxicity in non-tumor cells. Labeling of liposomes with Rhodamine allowed assessing internalization in cells, which showed significant cell uptake after 6 h of incubation. Cetuximab was used as targeting moiety in the PEGylated liposomes that displayed higher internalization rate in HCT116 cells when compared with non-targeted liposomes, which seems to internalize via active binding of Cetuximab to cells.

Conclusions

The proposed formulation open new avenues in the design of innovative transition metal-based vectorization systems that may be further extended to other novel metal complexes towards the improvement of their anti-cancer efficacy, which is usually hampered by solubility issues and/or toxicity to healthy tissues.

Notes

ACKNOWLEDGMENTS AND DISCLOSURES

We acknowledge Fundação para a Ciência e a Tecnologia (FCT/MEC) for financial support (Project PTDC/BBB-NAN/1812/2012; UCIBIO UID/Multi/04378/2013; UID/DTP/04138/2013). We thank M.Gajewska for MG85 synthesis and P. Borralho from iMed for Cetuximab.

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